UY32330A - NEW FORM OF SALT OF ACID 1- (4- {1- [E-4-CICLOHEXIL-3-TRIFLUORO-METIL-BENCILOXI-IMINO] -ETIL} -2-ETIL-BENCIL) -AZETIDIN-3-CARBOXYLICAL, POLYMODIC FORMS , PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, PREPARATION PROCESSES AND APPLICATIONS - Google Patents
NEW FORM OF SALT OF ACID 1- (4- {1- [E-4-CICLOHEXIL-3-TRIFLUORO-METIL-BENCILOXI-IMINO] -ETIL} -2-ETIL-BENCIL) -AZETIDIN-3-CARBOXYLICAL, POLYMODIC FORMS , PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, PREPARATION PROCESSES AND APPLICATIONSInfo
- Publication number
- UY32330A UY32330A UY0001032330A UY32330A UY32330A UY 32330 A UY32330 A UY 32330A UY 0001032330 A UY0001032330 A UY 0001032330A UY 32330 A UY32330 A UY 32330A UY 32330 A UY32330 A UY 32330A
- Authority
- UY
- Uruguay
- Prior art keywords
- etil
- salt
- pharmaceutical compositions
- azetidin
- imino
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 150000003839 salts Chemical class 0.000 title abstract 3
- 239000002253 acid Substances 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/15—Fumaric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Esta invención se refiere a una de hemi-fumarato del ácido 1-(4-{1-[(E)-4-ciclohexil-3-trifluoruro-metil-benciloxi-imino]-etil}-2-etil-bencil)-azetidin-3-carboxílico (Compuesto I), a composiciones farmacéuticas que comprenden esta sal, a procesos para formar esta sal, y su uso en un tratamiento médico. En adición, la presente invención también se refiere a nuevas formas polimórficas de la forma de sal de hemi-fumarato del Compuesto I. así como a composiciones farmacéuticas que comprenden estas formas polimórficas, a procesos para obtenerlas, y a su uso en un tratamiento médico.This invention relates to a 1- (4- {1 - [(E) -4-cyclohexyl-3-trifluoride-methyl-benzyloxy-imino] -ethyl} -2-ethyl-benzyl) - hemi-fumarate azetidin-3-carboxylic (Compound I), to pharmaceutical compositions comprising this salt, to processes to form this salt, and their use in medical treatment. In addition, the present invention also relates to novel polymorphic forms of the hemi-fumarate salt form of Compound I. as well as pharmaceutical compositions comprising these polymorphic forms, processes for obtaining them, and their use in medical treatment.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20305308P | 2008-12-18 | 2008-12-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UY32330A true UY32330A (en) | 2010-07-30 |
Family
ID=42236293
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UY0001032330A UY32330A (en) | 2008-12-18 | 2009-12-16 | NEW FORM OF SALT OF ACID 1- (4- {1- [E-4-CICLOHEXIL-3-TRIFLUORO-METIL-BENCILOXI-IMINO] -ETIL} -2-ETIL-BENCIL) -AZETIDIN-3-CARBOXYLICAL, POLYMODIC FORMS , PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, PREPARATION PROCESSES AND APPLICATIONS |
Country Status (35)
| Country | Link |
|---|---|
| US (7) | US20120115840A1 (en) |
| EP (2) | EP2676953B1 (en) |
| JP (1) | JP5627597B2 (en) |
| KR (5) | KR20110096584A (en) |
| CN (2) | CN102256943A (en) |
| AR (3) | AR074694A1 (en) |
| AU (1) | AU2009335924B2 (en) |
| BR (1) | BRPI0923176B8 (en) |
| CA (2) | CA2747437C (en) |
| CL (1) | CL2011001490A1 (en) |
| CO (1) | CO6390104A2 (en) |
| CY (2) | CY1114662T1 (en) |
| DK (2) | DK2676953T3 (en) |
| EC (1) | ECSP11011210A (en) |
| ES (2) | ES2631203T3 (en) |
| HR (2) | HRP20131106T1 (en) |
| HU (1) | HUE034819T2 (en) |
| IL (3) | IL253845B (en) |
| JO (1) | JO2894B1 (en) |
| LT (1) | LT2676953T (en) |
| MA (1) | MA32961B1 (en) |
| MX (1) | MX2011006609A (en) |
| MY (1) | MY152669A (en) |
| NZ (1) | NZ593061A (en) |
| PE (2) | PE20120336A1 (en) |
| PL (2) | PL2676953T3 (en) |
| PT (2) | PT2676953T (en) |
| RS (2) | RS53041B (en) |
| RU (1) | RU2518114C3 (en) |
| SG (1) | SG171785A1 (en) |
| SI (2) | SI2379497T1 (en) |
| TW (2) | TWI591055B (en) |
| UY (1) | UY32330A (en) |
| WO (1) | WO2010080409A1 (en) |
| ZA (1) | ZA201103709B (en) |
Families Citing this family (30)
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| UA114283C2 (en) * | 2011-01-07 | 2017-05-25 | Новартіс Аг | COMPOSITIONS OF IMMUNOSUPRESSANTS |
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| US20170027906A1 (en) | 2014-04-10 | 2017-02-02 | Philippe Michel Rene Bouillot | Immunosuppressant formulation |
| CN106456552A (en) * | 2014-04-10 | 2017-02-22 | 诺华股份有限公司 | Immediate Release Dosage Regimen for S1P Modulators |
| WO2016135644A1 (en) | 2015-02-26 | 2016-09-01 | Novartis Ag | Treatment of autoimmune disease in a patient receiving additionally a beta-blocker |
| EP3400211A1 (en) | 2016-01-04 | 2018-11-14 | Auspex Pharmaceuticals, Inc. | Azetidine modulators of the sphingosine 1-phosphate receptor |
| US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| US11434200B2 (en) | 2017-03-09 | 2022-09-06 | Novartis Ag | Solid forms comprising an oxime ether compound and a coformer, compositions and methods of use thereof |
| US11958805B2 (en) * | 2017-03-09 | 2024-04-16 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| MX2020007270A (en) * | 2017-09-27 | 2020-08-17 | Novartis Ag | Parenteral formulation comprising siponimod. |
| CN111405897A (en) | 2017-09-27 | 2020-07-10 | 雷迪博士实验室有限公司 | Process for the preparation of siponimod, its salts and solid forms |
| EP3687531A1 (en) | 2017-09-29 | 2020-08-05 | Novartis AG | Dosing regimen of siponimod |
| MX2020007268A (en) | 2017-09-29 | 2020-08-17 | Novartis Ag | Dosing regimen of siponimod. |
| WO2019144094A1 (en) | 2018-01-22 | 2019-07-25 | Teva Pharmaceuticals International Gmbh | Crystalline siponimod fumaric acid and polymorphs thereof |
| CN110776450B (en) * | 2018-07-27 | 2022-09-27 | 广东东阳光药业有限公司 | A kind of simpomod crystal form and preparation method thereof |
| KR20200072795A (en) | 2018-12-13 | 2020-06-23 | 고려대학교 산학협력단 | Pharmaceutical composition for preventing or treating circadian clock related disease comprising oxyiminomethylbenzene derivatives |
| CN111484434A (en) * | 2019-01-29 | 2020-08-04 | 东莞市东阳光仿制药研发有限公司 | A kind of simpomod crystal form and preparation method thereof |
| WO2020161632A1 (en) * | 2019-02-07 | 2020-08-13 | Dr. Reddy’S Laboratories Limited | Crystalline solid forms of siponimod |
| US20220144768A1 (en) * | 2019-02-27 | 2022-05-12 | Dr. Reddy's Laboratories Limited | Solid state forms of siponimod |
| EP3947370A4 (en) * | 2019-03-28 | 2022-12-28 | 1st Biotherapeutics, Inc. | PHARMACEUTICAL SALTS OF BENZOTHIAZOLE COMPOUNDS, POLYMORPHS AND PROCESSES FOR THEIR PRODUCTION |
| EP3972954A1 (en) | 2019-05-21 | 2022-03-30 | Synthon B.V. | Siponimod maleic acid and fumaric acid salt |
| CA3156298A1 (en) | 2019-10-31 | 2021-05-06 | Laetitia POUZOL | Combination of a cxcr7 antagonist with an s1p1 receptor modulator |
| GB202002560D0 (en) * | 2020-02-24 | 2020-04-08 | Johnson Matthey Plc | Crystalline forms of voxelotor, and processes for the preparation thereof |
| EP4139282A2 (en) * | 2020-05-29 | 2023-03-01 | Cipla Limited | Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof |
| EP4217341A1 (en) | 2020-09-25 | 2023-08-02 | Synthon B.V. | Siponimod salts and cocrystals |
| CN116456977A (en) * | 2020-09-25 | 2023-07-18 | 斯索恩有限公司 | Cinnimod salts and co-crystals |
| CN112402610A (en) * | 2020-11-20 | 2021-02-26 | 睿阜隆(杭州)生物医药有限公司 | New use of sphingosine-1-phosphate receptor modulator in preparation of medicine for treating diabetes |
| WO2022127863A1 (en) * | 2020-12-16 | 2022-06-23 | 苏州晶云药物科技股份有限公司 | Crystal forms of hemifumarate salt of carboxylic acid compound and preparation method therefor |
| US20240150282A1 (en) | 2021-03-26 | 2024-05-09 | Olon S.P.A. | Novel crystalline compound of siponimod hemifumarate |
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2009
- 2009-12-16 KR KR1020117016548A patent/KR20110096584A/en not_active Ceased
- 2009-12-16 KR KR1020167030350A patent/KR20160129915A/en not_active Ceased
- 2009-12-16 MY MYPI20112413 patent/MY152669A/en unknown
- 2009-12-16 EP EP13177190.9A patent/EP2676953B1/en active Active
- 2009-12-16 CA CA2747437A patent/CA2747437C/en active Active
- 2009-12-16 SI SI200930750T patent/SI2379497T1/en unknown
- 2009-12-16 PT PT131771909T patent/PT2676953T/en unknown
- 2009-12-16 SI SI200931675A patent/SI2676953T1/en unknown
- 2009-12-16 AU AU2009335924A patent/AU2009335924B2/en active Active
- 2009-12-16 KR KR1020187000381A patent/KR101885052B1/en not_active Expired - Fee Related
- 2009-12-16 CN CN2009801512748A patent/CN102256943A/en active Pending
- 2009-12-16 PE PE2011001226A patent/PE20120336A1/en not_active Application Discontinuation
- 2009-12-16 PE PE2014001111A patent/PE20142374A1/en not_active Application Discontinuation
- 2009-12-16 IL IL253845A patent/IL253845B/en unknown
- 2009-12-16 MX MX2011006609A patent/MX2011006609A/en active IP Right Grant
- 2009-12-16 KR KR1020167013818A patent/KR20160064245A/en not_active Ceased
- 2009-12-16 DK DK13177190.9T patent/DK2676953T3/en active
- 2009-12-16 JP JP2011542351A patent/JP5627597B2/en active Active
- 2009-12-16 CN CN201510102280.1A patent/CN104803902A/en active Pending
- 2009-12-16 LT LTEP13177190.9T patent/LT2676953T/en unknown
- 2009-12-16 HR HRP20131106AT patent/HRP20131106T1/en unknown
- 2009-12-16 KR KR1020177014691A patent/KR20170062554A/en not_active Ceased
- 2009-12-16 RU RU2011129222A patent/RU2518114C3/en active Protection Beyond IP Right Term
- 2009-12-16 NZ NZ593061A patent/NZ593061A/en not_active IP Right Cessation
- 2009-12-16 RS RS20130510A patent/RS53041B/en unknown
- 2009-12-16 PL PL13177190T patent/PL2676953T3/en unknown
- 2009-12-16 US US13/140,478 patent/US20120115840A1/en not_active Abandoned
- 2009-12-16 ES ES13177190.9T patent/ES2631203T3/en active Active
- 2009-12-16 UY UY0001032330A patent/UY32330A/en not_active Application Discontinuation
- 2009-12-16 DK DK09793413.7T patent/DK2379497T3/en active
- 2009-12-16 PL PL09793413T patent/PL2379497T3/en unknown
- 2009-12-16 SG SG2011036886A patent/SG171785A1/en unknown
- 2009-12-16 PT PT97934137T patent/PT2379497E/en unknown
- 2009-12-16 IL IL294514A patent/IL294514A/en unknown
- 2009-12-16 EP EP09793413.7A patent/EP2379497B1/en active Active
- 2009-12-16 MA MA34008A patent/MA32961B1/en unknown
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2011
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2013
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2015
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2017
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2018
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2020
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2021
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2022
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2024
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